Anti-diabetic potential of Viburnum betulifolium fruits: Sesquilignans with α-amylase, α-glucosidase, and PTP1B inhibitory activities

• Published in: Industrial crops and products Vol. 187; p. 115362
• Main Authors: Chen, Jia, Tang, Yi-Yuan, Zhao, Chun-Chao, Zhang, Xiao-Hui, Li, Shi-Xin, Shao, Jian-Hua
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.11.2022
• Subjects: Enzyme inhibition; Hypoglycemic effect; Molecular modeling; Sesquilignan; Viburnum betulifolium fruits; Enzyme inhibition; Viburnum betulifolium fruits; Sesquilignan; Hypoglycemic effect; Molecular modeling
• ISSN: 0926-6690; 1872-633X
• DOI: 10.1016/j.indcrop.2022.115362

Viburnum betulifolium Batal. is an incredibly attractive and widely cultivated plant due to the great industrial value of its fruits, flowers, roots, stems, and barks. In this study, the MeOH extract of Viburnum betulifolium fruits (VBFM) was first reported to show obvious hypoglycemic effects in diabetic and normal mice, and it exhibited weak inhibitory effect on α-amylase and significant inhibition against α-glucosidase and PTP1B. In order to elucidate the anti-diabetic components, six undescribed sesquilignans, vibetulifols A−F (1−6), one new natural sesquilignan 9, and three known analogues (7, 8, and 10) were isolated from VBFM by bioactivity-guided fractionation and identified by extensive spectroscopic analyses. Compounds 1−8 exhibited moderate inhibitory effects on α-amylase with IC50 values ranging from 35.10 to 51.52 μM, and compounds 1−3 and 6 displayed significant α-glucosidase inhibitory effects (IC50 = 5.17, 6.73, 3.05, and 15.37 μM, respectively), while compounds 3 and 4 also displayed potent PTP1B inhibitory activities (IC50 = 3.29 and 3.15 μM, respectively) and good selectivity over TCPTP. Furthermore, the enzyme kinetic studies and molecular modeling analyses for compounds 3 and 4 were also performed. These results could provide scientific guidance and foundation for the further development and utilization of V. betulifolium fruits in pharmaceutical industry. [Display omitted] •This study first evaluated the anti-diabetic potential of V. betulifolium fruits.•Ten sesquilignans including six undescribed were isolated from V. betulifolium fruits.•Some of the sesquilignans showed potent inhibition of both α-glucosidase and PTP1B.•Compounds 3 and 4 exhibited obvious selective inhibition against PTP1B over TCPTP.•Molecular modeling studies of 3 and 4 supported the experimental observations.